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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Cell Cycle > PHA-793887CAS：718630-59-2
Molecular Formula：C19H31N5O2
Molecular Weight：361.48
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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| CAS | 718630-59-2 |
| Name | PHA-793887 |
| Molecular Formula | C19H31N5O2 |
| Molecular Weight | 361.48 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD17169992 |
| SMILES | CC(C)CC(NC1=NNC2=C1CN(C(C3CCN(C)CC3)=O)C2(C)C)=O |
| Target Point | CDK |
| Passage | Cell Cycle |
| Background | PHA-793887 is a potent, ATP-competitive CDK inhibitor. |
| Biological Activity | PHA-793887 是一种有效的, ATP 竞争性的 CDK 抑制剂, 可抑制 Cdk2, Cdk1, Cdk4 和 Cdk9 的活性, IC50 值分别为 8 nM, 60 nM, 62 nM 和 138 nM, 同时可抑制糖原合酶激酶 3β (GSK-3β) , IC50 值为 79 nM。[1-4] |
| IC50 | Cdk5/p25:5nM (IC50) cdk2/cyclin A:8nM (IC50) CDK2/cyclinE:8nM (IC50) CDK7/cyclin H:10nM (IC50) Cdk1/cyclin B:60nM (IC50) Cdk4/cyclin D1:62nM (IC50) CDK9/cyclinT1:138nM (IC50) GSK-3β:79nM (IC50) [1-4] |
| Data Literature Source | [1]. Locatelli G， et al. Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study. Mol Cancer Ther. 2010 May; 9 (5) :1265-73. [2]. Massard C， et al. A first in man， phase I dose-escalation study of PHA-793887， an inhibitor of multiple cyclin-dependent kinases (CDK2， 1 and 4) reveals unexpected hepatotoxicity in patients with solid tumors. Cell Cycle. 2011 Mar 15; 10 (6) :963-70. Epub 2011 Mar 15. [3]. Alzani R， et al. Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models. Exp Hematol. 2010 Apr; 38 (4) :259-269.e2. [4]. Brasca MG， et al. Optimization of 6，6-dimethyl pyrrolo[3，4-c]pyrazoles: Identification of PHA-793887， a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1; 18 (5) :1844-53. |
| Unit | Bottle |
| Specification | 2mg 10mM*1mL in DMSO 5mg 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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